AR129934A1 - MACROCYCLIC COMPOUNDS FOR CANCER TREATMENT - Google Patents
MACROCYCLIC COMPOUNDS FOR CANCER TREATMENTInfo
- Publication number
- AR129934A1 AR129934A1 ARP230101857A ARP230101857A AR129934A1 AR 129934 A1 AR129934 A1 AR 129934A1 AR P230101857 A ARP230101857 A AR P230101857A AR P230101857 A ARP230101857 A AR P230101857A AR 129934 A1 AR129934 A1 AR 129934A1
- Authority
- AR
- Argentina
- Prior art keywords
- cancer
- 6alkyl
- compound according
- 6haloalkyl
- morpholinyl
- Prior art date
Links
- 206010028980 Neoplasm Diseases 0.000 title abstract 5
- 201000011510 cancer Diseases 0.000 title abstract 5
- 238000011282 treatment Methods 0.000 title abstract 3
- 150000002678 macrocyclic compounds Chemical class 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 6
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 5
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 abstract 2
- 102000010400 1-phosphatidylinositol-3-kinase activity proteins Human genes 0.000 abstract 2
- 206010009944 Colon cancer Diseases 0.000 abstract 2
- 208000001333 Colorectal Neoplasms Diseases 0.000 abstract 2
- 206010069755 K-ras gene mutation Diseases 0.000 abstract 2
- 108091007960 PI3Ks Proteins 0.000 abstract 2
- 239000012636 effector Substances 0.000 abstract 2
- 229910052736 halogen Inorganic materials 0.000 abstract 2
- 150000002367 halogens Chemical class 0.000 abstract 2
- 230000002401 inhibitory effect Effects 0.000 abstract 2
- 125000002757 morpholinyl group Chemical group 0.000 abstract 2
- 238000011321 prophylaxis Methods 0.000 abstract 2
- 125000003161 (C1-C6) alkylene group Chemical group 0.000 abstract 1
- GOJUJUVQIVIZAV-UHFFFAOYSA-N 2-amino-4,6-dichloropyrimidine-5-carbaldehyde Chemical group NC1=NC(Cl)=C(C=O)C(Cl)=N1 GOJUJUVQIVIZAV-UHFFFAOYSA-N 0.000 abstract 1
- -1 3-oxo-5,6,8,8a-tetrahydro-1H-imidazo[5,1-c][1,4]oxazinyl Chemical group 0.000 abstract 1
- 206010052747 Adenocarcinoma pancreas Diseases 0.000 abstract 1
- 206010014733 Endometrial cancer Diseases 0.000 abstract 1
- 206010014759 Endometrial neoplasm Diseases 0.000 abstract 1
- 208000000461 Esophageal Neoplasms Diseases 0.000 abstract 1
- 208000022072 Gallbladder Neoplasms Diseases 0.000 abstract 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 abstract 1
- 102000043136 MAP kinase family Human genes 0.000 abstract 1
- 108091054455 MAP kinase family Proteins 0.000 abstract 1
- 206010030155 Oesophageal carcinoma Diseases 0.000 abstract 1
- 206010033128 Ovarian cancer Diseases 0.000 abstract 1
- 206010061535 Ovarian neoplasm Diseases 0.000 abstract 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 abstract 1
- 125000002393 azetidinyl group Chemical group 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 201000004101 esophageal cancer Diseases 0.000 abstract 1
- 201000010175 gallbladder cancer Diseases 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- 230000003993 interaction Effects 0.000 abstract 1
- 201000005202 lung cancer Diseases 0.000 abstract 1
- 208000020816 lung neoplasm Diseases 0.000 abstract 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 abstract 1
- 201000001441 melanoma Diseases 0.000 abstract 1
- 208000002154 non-small cell lung carcinoma Diseases 0.000 abstract 1
- 231100000590 oncogenic Toxicity 0.000 abstract 1
- 230000002246 oncogenic effect Effects 0.000 abstract 1
- 201000002094 pancreatic adenocarcinoma Diseases 0.000 abstract 1
- 201000002528 pancreatic cancer Diseases 0.000 abstract 1
- 208000008443 pancreatic carcinoma Diseases 0.000 abstract 1
- 125000004193 piperazinyl group Chemical group 0.000 abstract 1
- 125000003386 piperidinyl group Chemical group 0.000 abstract 1
- 230000001902 propagating effect Effects 0.000 abstract 1
- 102000016914 ras Proteins Human genes 0.000 abstract 1
- 102200006531 rs121913529 Human genes 0.000 abstract 1
- 102200006539 rs121913529 Human genes 0.000 abstract 1
- 102200006538 rs121913530 Human genes 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 230000011664 signaling Effects 0.000 abstract 1
- 125000005557 thiazolylene group Chemical group 0.000 abstract 1
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/22—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains four or more hetero rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Epidemiology (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
Reivindicación 1: Un compuesto de fórmula (1), en donde R¹ es un resto de fórmula (2), 3-oxo-5,6,8,8a-tetrahidro-1H-imidazo[5,1-c][1,4]oxazinilo o (alquil C₁₋₆)oxoimidazolidinilo; en donde R⁸ es alquil C₁₋₆; R⁹ es ((alquil C₁₋₆)₂amino)azetidinilo, alquilpiperazinil C₁₋₆, haloazetidinilo, haloalquilamino C₁₋₆, haloalquilaminoazetidinil C₁₋₆, haloalquilpiperazinil C₁₋₆, hidroxi(alquil C₁₋₆)piperidinilo o morfolinilo; R² es alquil C₁₋₆; R³ es H o halógeno; R⁴ es H o halógeno; R⁵ es alquil C₁₋₆ o haloalquil C₁₋₆; R⁶ es alcoxi C₁₋₆alquil C₁₋₆; R⁷ es morfolinilo, (haloalquil C₁₋₆)piperazinilo o alquilpiperazinil C₁₋₆; A¹ es tiazolileno; A² es alquilen C₁₋₆; siempre que R³ y R⁴ no sean H en simultáneo; o una sal farmacéuticamente aceptable de este. Reivindicación 25: El uso de un compuesto de acuerdo con cualquiera de las reivindicaciones 1 a 20 para tratar una enfermedad relacionada con la proteína KRAS G12C, G12D y G12V. Reivindicación 26: El uso de un compuesto de acuerdo con cualquiera de las reivindicaciones 1 a 20 para inhibir la interacción de RAS con efectores corriente abajo, en donde los efectores corriente abajo son RAF y PI3K. Reivindicación 27: El uso de un compuesto de acuerdo con cualquiera de las reivindicaciones 1 a 20 para inhibir la señalización de MAPK y PI3K oncogénicas en propagación. Reivindicación 28: El uso de un compuesto de acuerdo con cualquiera de las reivindicaciones 1 a 20 para el tratamiento o profilaxis de tipos de cáncer causados por mutación de KRAS, en donde el cáncer se selecciona de cáncer pancreático, cáncer colorrectal, cáncer de pulmón, cáncer de esófago, cáncer de vesícula biliar, cáncer de ovario melanoma y cáncer endométrico. Reivindicación 29: El uso de un compuesto de acuerdo con cualquiera de las reivindicaciones 1 a 20 para el tratamiento o profilaxis de tipos de cáncer causados por mutación de KRAS, en donde el cáncer se selecciona de adenocarcinoma pancreático, cáncer colorrectal y cáncer de pulmón no microcítico.Claim 1: A compound of formula (1), wherein R¹ is a moiety of formula (2), 3-oxo-5,6,8,8a-tetrahydro-1H-imidazo[5,1-c][1,4]oxazinyl or (C₁₋₆alkyl)oxoimidazolidinyl; wherein R⁸ is C₁₋₆alkyl; R⁹ is ((C₁₋₆alkyl)₂amino)azetidinyl, C₁₋₆alkylpiperazinyl, haloazetidinyl, C₁₋₆haloalkylamino, C₁₋₆haloalkylaminoazetidinyl, C₁₋₆haloalkylpiperazinyl, hydroxy(C₁₋₆alkyl)piperidinyl or morpholinyl; R² is C₁₋₆alkyl; R³ is H or halogen; R⁴ is H or halogen; R⁵ is C₁₋₆alkyl or C₁₋₆haloalkyl; R⁶ is C₁₋₆alkoxyC₁₋₆alkyl; R⁷ is morpholinyl, (C₁₋₆haloalkyl)piperazinyl or C₁₋₆alkylpiperazinyl; A¹ is thiazolylene; A² is C₁₋₆alkylene; provided that R³ and R⁴ are not simultaneously H; or a pharmaceutically acceptable salt thereof. Claim 25: The use of a compound according to any one of claims 1 to 20 for treating a disease related to KRAS G12C, G12D and G12V protein. Claim 26: The use of a compound according to any one of claims 1 to 20 for inhibiting the interaction of RAS with downstream effectors, wherein the downstream effectors are RAF and PI3K. Claim 27: The use of a compound according to any one of claims 1 to 20 for inhibiting propagating oncogenic MAPK and PI3K signaling. Claim 28: The use of a compound according to any one of claims 1 to 20 for the treatment or prophylaxis of cancer types caused by KRAS mutation, wherein the cancer is selected from pancreatic cancer, colorectal cancer, lung cancer, esophageal cancer, gallbladder cancer, ovarian cancer melanoma and endometrial cancer. Claim 29: The use of a compound according to any one of claims 1 to 20 for the treatment or prophylaxis of cancer types caused by KRAS mutation, wherein the cancer is selected from pancreatic adenocarcinoma, colorectal cancer and non-small cell lung cancer.
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2022106792 | 2022-07-20 | ||
| CN2022128979 | 2022-11-01 | ||
| CN2023070766 | 2023-01-05 | ||
| CN2023087631 | 2023-04-11 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR129934A1 true AR129934A1 (en) | 2024-10-16 |
Family
ID=87514141
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP230101857A AR129934A1 (en) | 2022-07-20 | 2023-07-14 | MACROCYCLIC COMPOUNDS FOR CANCER TREATMENT |
Country Status (8)
| Country | Link |
|---|---|
| KR (1) | KR20250034953A (en) |
| CN (1) | CN119585284A (en) |
| AR (1) | AR129934A1 (en) |
| AU (1) | AU2023311244A1 (en) |
| CO (1) | CO2025001184A2 (en) |
| IL (1) | IL316706A (en) |
| TW (1) | TWI860785B (en) |
| WO (1) | WO2024017859A1 (en) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AR127308A1 (en) | 2021-10-08 | 2024-01-10 | Revolution Medicines Inc | RAS INHIBITORS |
| EP4469164A1 (en) | 2023-02-14 | 2024-12-04 | F. Hoffmann-La Roche AG | Tricyclic compounds for the treatment of cancer |
| WO2024206858A1 (en) | 2023-03-30 | 2024-10-03 | Revolution Medicines, Inc. | Compositions for inducing ras gtp hydrolysis and uses thereof |
| WO2024211663A1 (en) | 2023-04-07 | 2024-10-10 | Revolution Medicines, Inc. | Condensed macrocyclic compounds as ras inhibitors |
| WO2024211712A1 (en) | 2023-04-07 | 2024-10-10 | Revolution Medicines, Inc. | Condensed macrocyclic compounds as ras inhibitors |
| WO2024229406A1 (en) | 2023-05-04 | 2024-11-07 | Revolution Medicines, Inc. | Combination therapy for a ras related disease or disorder |
| WO2025034702A1 (en) | 2023-08-07 | 2025-02-13 | Revolution Medicines, Inc. | Rmc-6291 for use in the treatment of ras protein-related disease or disorder |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20220218852A1 (en) | 2019-04-18 | 2022-07-14 | Provincial Health Services Authority | Novel radiolabelled cxcr4-targeting compounds for diagnosis and therapy |
| TW202132314A (en) * | 2019-11-04 | 2021-09-01 | 美商銳新醫藥公司 | Ras inhibitors |
| KR20230067635A (en) * | 2020-09-15 | 2023-05-16 | 레볼루션 메디슨즈, 인크. | Indole derivatives as RAS inhibitors in the treatment of cancer |
-
2023
- 2023-07-14 AR ARP230101857A patent/AR129934A1/en unknown
- 2023-07-18 KR KR1020257001146A patent/KR20250034953A/en active Pending
- 2023-07-18 CN CN202380054201.7A patent/CN119585284A/en active Pending
- 2023-07-18 WO PCT/EP2023/069851 patent/WO2024017859A1/en active Application Filing
- 2023-07-18 IL IL316706A patent/IL316706A/en unknown
- 2023-07-18 AU AU2023311244A patent/AU2023311244A1/en active Pending
- 2023-07-19 TW TW112126951A patent/TWI860785B/en active
-
2025
- 2025-01-31 CO CONC2025/0001184A patent/CO2025001184A2/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| WO2024017859A1 (en) | 2024-01-25 |
| CO2025001184A2 (en) | 2025-02-13 |
| KR20250034953A (en) | 2025-03-11 |
| AU2023311244A1 (en) | 2024-11-14 |
| IL316706A (en) | 2024-12-01 |
| TW202413378A (en) | 2024-04-01 |
| TWI860785B (en) | 2024-11-01 |
| CN119585284A (en) | 2025-03-07 |
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